title: Novel promising linezolid analogues: rational design, synthesis and biological evaluation.
abstract: A new series of 5-substituted oxazolidinones derived from linezolid, having urea and thiourea moieties at the C-5 side chain of the oxazolidinone ring, were prepared and their in vitro antibacterial activity was evaluated. The compound 10f demonstrated high antimicrobial activity, comparable to that of linezolid against Staphylococcus aureus.
authors.affiliation: Dipartimento di Chimica e Biologia, Università degli Studi di Salerno, via Giovanni Paolo II, 132, 84084 Fisciano, SA, Italy.
authors.forename: Margherita
authors.initials: M
authors.lastname: De Rosa
authors.forename: Anna
authors.initials: A
authors.lastname: Zanfardino
authors.forename: Eugenio
authors.initials: E
authors.lastname: Notomista
authors.forename: Thomas A
authors.initials: TA
authors.lastname: Wichelhaus
authors.forename: Carmela
authors.initials: C
authors.lastname: Saturnino
authors.forename: Mario
authors.initials: M
authors.lastname: Varcamonti
authors.forename: Annunziata
authors.initials: A
authors.lastname: Soriente
mesh_terms: D000081:Acetamides / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D000900:Anti-Bacterial Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D004305:Dose-Response Relationship, Drug; D015195:Drug Design; D000069349:Linezolid; D008826:Microbial Sensitivity Tests; D015394:Molecular Structure; D023303:Oxazolidinones / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D013211:Staphylococcus aureus / Q000166:cytology / Q000187:drug effects*; D013329:Structure-Activity Relationship
chemical_list: D000081:Acetamides; D000900:Anti-Bacterial Agents; D023303:Oxazolidinones; D000069349:Linezolid
keywords: Antibacterial; Linezolid; Oxazolidinone; Structure–activity relationship; Thiourea